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1. 发明申请

US20060142598A1 Process for producing benzofuran derivative 失效
标题翻译：苯并呋喃衍生物的制备方法
公开(公告)号：US20060142598A1
公开(公告)日：2006-06-29
申请号：US11359023
申请日：2006-02-22
申请人： Hiroyuki Tawada , Makoto Yamashita , Yujiro Ono
发明人： Hiroyuki Tawada , Makoto Yamashita , Yujiro Ono
IPC分类号： C07D493/00
CPC分类号： C07D307/79 , Y02P20/55
摘要： A novel process for efficiently and easily producing a compound represented by the formula: wherein ring A is a benzene ring that may be optionally further substituted in addition to the group represented by W, or a salt thereof; which comprises reacting a compound represented by the formula: wherein R1 and R2 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, Y is a halogen atom, ring A is a benzene ring that may be optionally further substituted in addition to the group represented by Y and ring B is an optionally substituted benzene ring, or a salt thereof, with a compound represented by the formula: WH wherein W is wherein ring C is an optionally substituted benzene ring, ring D is an optionally substituted 5- to 7-membered nitrogen-containing heterocyclic ring, R3 is a hydrogen atom, an aliphatic hydrocarbon group containing an aromatic group or an acyl group, and R4 is a hydrogen atom, an optionally substituted hydrocarbon group or an acyl group, or a salt thereof and thereafter, if necessary, deprotecting the resultant product, which is suitable for industrial production.
摘要翻译：一种用于有效且容易地制备由下式表示的化合物的新方法：其中环A是可以任选进一步被W代表的基团进一步取代的苯环或其盐; 其包括使下式表示的化合物：其中R 1和R 2彼此相同或不同，并且各自为氢原子，任选取代的烃基或任选地取代的杂环基，Y是卤素原子，环A是可以任选地进一步被Y代表的基团进一步取代的苯环，并且环B是任选取代的苯环或其盐与由式中W为W，其中环C为任选取代的苯环，环D为任选取代的5至7元含氮杂环，R 3为氢原子，含有芳基或酰基的脂族烃基，R 4为氢原子，任选取代的烃基或酰基，或其盐，然后如果需要，将所得物产品，适用于工业产品说明。

2. 发明申请

US20050171184A1 Process for preparing optically active 2,3-dihydrobenzofuran compounds 失效
标题翻译：光学活性2,3-二氢苯并呋喃化合物的制备方法
公开(公告)号：US20050171184A1
公开(公告)日：2005-08-04
申请号：US11054371
申请日：2005-02-09
申请人： Isao Aoki , Mari Adachi , Hiroyuki Tawada , Makoto Yamashita , Misayo Sera
发明人： Isao Aoki , Mari Adachi , Hiroyuki Tawada , Makoto Yamashita , Misayo Sera
IPC分类号： C07D307/79 , C07D405/04 , C07F9/6574 , A61K31/4035 , C07D45/02
CPC分类号： C07D307/79 , C07B2200/07 , C07D405/04 , C07F9/65742
摘要： A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.
摘要翻译：一种制备光学活性2,3-二氢苯并呋喃化合物的方法，其包括用光学活性酸化合物对其进行光学拆分的2,3-二氢苯并呋喃化合物或其盐进行光学拆分：其中R 1， SUP>和R 2各自为氢或任选取代的烃基; R 3是任选取代的芳族基团; 并且C是除了氨基之外还可以具有取代基的苯环]。该方法可以在工业上有利地生产用于合成可用作神经变性疾病等的预防和/或治疗药物的光学活性2,3-二氢苯并呋喃化合物的中间体。

3. 发明授权

US06414003B1 Oxazolone derivatives and their use as anti-helicobacter pylori agents 失效
标题翻译：恶唑酮衍生物及其作为幽门螺杆菌药物的用途
公开(公告)号：US06414003B1
公开(公告)日：2002-07-02
申请号：US09708542
申请日：2000-11-09
申请人： Tsuneo Kanamaru , Masafumi Nakao , Hiroyuki Tawada , Keiji Kamiyama
发明人： Tsuneo Kanamaru , Masafumi Nakao , Hiroyuki Tawada , Keiji Kamiyama
IPC分类号： A61K31422
CPC分类号： C07D413/06 , C07D263/48 , C07D413/14 , C07D471/04 , C12P17/16
摘要： An anti-Helicobacter pylori agent comprising a compound represented by the formula: wherein A represents an aromatic ring group which may be substituted; R1 and R2, whether identical or not, each represent a hydrogen atom or a hydrocarbon group which may be substituted; R3 and R4, whether identical or not, each represent a hydrogen atom, a hydrocarbon group which may be substituted, an acyl group, a carbamoyl group which may be substituted, or a carboxyl group which may be esterified; or a salt thereof.
摘要翻译：一种抗幽门螺杆菌药物，其包含由下式表示的化合物：其中A表示可被取代的芳族环基团; R1和R2各自表示氢原子或可被取代的烃基; R 3和R 4各自表示氢原子，可被取代的烃基，酰基，可被取代的氨基甲酰基或可被酯化的羧基; 或其盐。

4. 发明授权

US06403595B1 Sulfonamide derivatives, processes for producing the same and utilization thereof 失效
标题翻译：磺酰胺衍生物，其制备方法及其利用
公开(公告)号：US06403595B1
公开(公告)日：2002-06-11
申请号：US09601660
申请日：2000-08-03
申请人： Hiroyuki Tawada , Fumio Itoh , Hiroshi Banno , Zen-ichi Terashita
发明人： Hiroyuki Tawada , Fumio Itoh , Hiroshi Banno , Zen-ichi Terashita
IPC分类号： A61K31495
CPC分类号： C07D231/12 , C07D233/56 , C07D241/08 , C07D243/08 , C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/12
摘要： The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which have activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.
摘要翻译：本发明提供由下式表示的化合物或其盐：其中R1是任选取代的烃基或任选取代的杂环基，环A是任选取代的二价含氮杂环基，X'是任选取代的亚烷基链，Y是任选取代的二价环基，X是化学键或任选取代的亚烷基链，Z是（1）任选取代的氨基，（2）任选取代的亚氨基或（3）任选取代的含氮杂环基或其前体药物，其具有活化的凝血因子X抑制活性并且可用作抗凝血剂。

5. 发明授权

US5278186A Chromene derivatives, their production and use 失效
标题翻译：色烯衍生物，其生产和使用
公开(公告)号：US5278186A
公开(公告)日：1994-01-11
申请号：US671796
申请日：1991-04-02
申请人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
发明人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
IPC分类号： C07D311/12 , C07D311/14 , C07D311/16 , C07D335/06 , A61F31/355
CPC分类号： C07D335/06 , C07D311/12 , C07D311/14 , C07D311/16
摘要： A chromene derivative of the formula (I) ##STR1## wherein each ring of A and B can have one or more substituents; X is an oxygen atom or sulfur atom, Y is an oxygen or sulfur atom or H.sub.2, Z is a bond, --NH-- or a saturated or unsaturated lower alkylene group and R is a hydrocarbon radical which is unsubstituted or substituted, or its salt, which is useful as a drug for atherosclerosis.
摘要翻译： PCT No.PCT / JP91 / 00172 Sec。 371日期：1991年4月2日 102（e）日期1991年4月2日PCT 1991年2月2日PCT PCT。公开号WO91 / 12249 日期：1991年8月22日。A和B的每个环可具有一个或多个取代基的式（I）的色烯衍生物（*化学结构*）（I） X是氧原子或硫原子，Y是氧或硫原子或H 2，Z是键，-NH-或饱和或不饱和的低级亚烷基，R是未取代或取代的烃基，或其盐，其可用作动脉粥样硬化的药物。

6. 发明授权

US4082764A Methods for the production of 4H-s-triazolo[4,3-a][1,4]benzodiazepine 5N-oxides 失效
标题翻译：生产4H-S-三唑（4,3-A）+8,1,4）苯并咪唑5N-氧化物的方法
公开(公告)号：US4082764A
公开(公告)日：1978-04-04
申请号：US612745
申请日：1975-09-12
申请人： Yutaka Kuwada , Kanji Meguro , Hiroyuki Tawada
发明人： Yutaka Kuwada , Kanji Meguro , Hiroyuki Tawada
IPC分类号： A61K20060101 , A61K31/55 , C07D20060101 , C07D239/92 , C07D243/00 , C07D249/00 , C07D249/08 , C07D487/04
CPC分类号： C07D239/92 , C07D249/08 , C07D487/04
摘要： The title compounds are prepared by reacting a 3-amino-3,4-dihydro-4-hydroxy-4-phenylquinazoline with a reactive derivative of a halogenoacetic acid, reacting the resultant halogenoacetyl derivative with a weak acid, reacting the resultant 2-(3-halomethyl-s-triazol-4-yl)benzophenone with hydroxylamine and subjecting the resultant 2-(3-hydroxyamino-methyl-s-triazol-4-yl)benzophenone to dehydration to effect ring closure.

7. 发明授权

US4002638A Benzazepine derivatives 失效
标题翻译：苯扎西平衍生物
公开(公告)号：US4002638A
公开(公告)日：1977-01-11
申请号：US505088
申请日：1974-09-11
申请人： Yutaka Kuwada , Hiroyuki Tawada , Kanji Meguro
发明人： Yutaka Kuwada , Hiroyuki Tawada , Kanji Meguro
IPC分类号： C07D487/04 , C07D249/12
CPC分类号： C07D487/04 , Y10S514/906 , Y10S514/96
摘要： Novel benzazepine derivatives of the formula ##STR1## wherein ring A is unsubstituted or substituted by halogen, nitro, alkyl, alkoxy or trifluoromethyl, R is hydrogen or alkyl which may be substituted, X is oxygen or sulfur and Y is -CH.sub.2 -CH.sub.2 - or -CH=CH-, and their pharmaceutically acceptable salts, exhibit excellent pharmacological activities such as analgetic and muscle relaxing activities.
摘要翻译：式A的新的苯并氮杂衍生物，其中环A未被取代或被卤素，硝基，烷基，烷氧基或三氟甲基取代，R是氢或可被取代的烷基，X是氧或硫，Y是-CH 2 -CH 2 - 或-CH = CH-及其药学上可接受的盐，表现出优异的药理活性，例如止痛和肌肉松弛活性。

8. 发明申请

US20070197636A1 Coumarin Derivative And Use Thereof 失效
标题翻译：香豆素衍生物及其用途
公开(公告)号：US20070197636A1
公开(公告)日：2007-08-23
申请号：US10591561
申请日：2005-03-01
申请人： Shogo Marui , Masaki Ogino , Hiroyuki Tawada , Osamu Yabe
发明人： Shogo Marui , Masaki Ogino , Hiroyuki Tawada , Osamu Yabe
IPC分类号： A61K31/366 , C07D311/02
CPC分类号： C07D311/16
摘要： The present invention relates to an alkaline earth metal salt or an organic amine salt of a compound represented by the formula : wherein R1 and R2 are each a hydrogen atom, a halogen atom, or an optionally substituted linear hydrocarbon group; ring A is an optionally further substituted benzene ring; B is an optionally substituted benzene ring; R is a carboxyl group or a linear hydrocarbon group substituted with a carboxyl group and the like.
摘要翻译：本发明涉及由下式表示的化合物的碱土金属盐或有机胺盐：其中R 1和R 2各自为氢原子，卤素原子或任选取代的直链烃基; 环A是任选进一步取代的苯环; B是任选取代的苯环; R是羧基或被羧基等取代的直链烃基。

9. 发明授权

US06784314B2 Process for producing amine derivatives 失效
标题翻译：制备胺衍生物的方法
公开(公告)号：US06784314B2
公开(公告)日：2004-08-31
申请号：US10240574
申请日：2002-10-01
申请人： Makoto Yamashita , Kaneyoshi Kato , Hiroyuki Tawada
发明人： Makoto Yamashita , Kaneyoshi Kato , Hiroyuki Tawada
IPC分类号： C07C23305
CPC分类号： C07C235/34 , C07B2200/07 , C07C217/74 , C07C2602/10
摘要： This invention provides a convenient and industrially advantageous process producing amine derivatives having the action of inhibiting the secretion and accumulation of amyloid &bgr; protein. In Compound (I), the ether linkage is selectively cleaved without cleaving the amide linkage present in the same molecule and tertiary amines are not converted into quaternary salts, and thus Amine Derivative (V) with good qualities having the action of inhibiting the secretion and accumulation of amyloid &bgr; protein can be obtained in high yield.
摘要翻译：本发明提供了方便和工业上有利的方法，产生具有抑制淀粉样蛋白β蛋白分泌和积累作用的胺衍生物。在化合物（I）中，醚键被选择性地切割而不裂解同一分子中存在的酰胺键和叔胺不会转化为季盐，因此可以高产率获得具有抑制淀粉样β蛋白分泌和积累作用的具有良好品质的胺衍生物（V）。

10. 发明授权

US06699995B1 Process for the preparation of oxazole derivatives 失效
标题翻译：恶唑衍生物的制备方法
公开(公告)号：US06699995B1
公开(公告)日：2004-03-02
申请号：US10088415
申请日：2002-03-18
申请人： Hiroyuki Tawada , Norihiko Ohashi , Motoki Ikeuchi
发明人： Hiroyuki Tawada , Norihiko Ohashi , Motoki Ikeuchi
IPC分类号： C07D26304
CPC分类号： C07D413/04 , C07D263/38 , C07D263/48
摘要： A production method of a compound represented by the formula wherein R1 and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R3 is an electron-withdrawing group, and R4, R5 and R6 are each a hydrogen atom or an optionally substituted hydrocarbon group, or a salt thereof, is provided as an industrially advantageous production. method for forming a carbon-carbon bond at the 5-position of oxazole, which method includes reacting a compound represented by the formula wherein the symbols in the formula are as defined above, or a salt thereof, with a compound represented by the formula wherein the symbols in the formula are as defined above, or a salt thereof, in the presence of an acid or a base.
摘要翻译：由式R 1和R 2表示的化合物的制备方法各自为氢原子，任选取代的烃基或任选取代的杂环基，R 3为吸电子基团，R 作为工业上有利的生产，提供了R 5和R 6各自为氢原子或任选取代的烃基或其盐。在恶唑的5-位上形成碳 - 碳键的方法，该方法包括使式中的符号表示的化合物或其盐与式中的化合物或其盐与式在式中如上所定义，或其盐在酸或碱的存在下进行。

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